MG 149
(Synonyms: Tip60 HAT inhibitor) 目录号 : GC11439
A HAT inhibitor
Cas No.:1243583-85-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Kinase experiment [1]: | |
|
Binding assays |
Radioisotope-labeled acetyltransferase assays were carried out at 30°C in a reaction volume of 30 μL. The reaction buffer contained 50 mM HEPES at pH 8.0, 0.1 mM EDTA, 50 μg/mL BSA, 1 mM dithiothreitol, 0.1% Triton-X100, and 2% DMSO. 14C-labeled Ac-CoA was used as the acetyl donor. The peptide containing the N-terminal 20-amino acid sequence of histone H4 (i.e. H4-20) was used as substrate for p300 and Tip60, and the peptide containing the N-terminal 20-amino acid sequence of histone H3 (i.e. H3-20) was employed as substrate for PCAF. The HAT reaction was initiated with the HAT enzyme after the other components (Ac-CoA, peptide substrate, and the inhibitor) were equilibrated at 30°C for 5 min. After the reaction, the mixture was loaded onto a Waterman P81 filter paper and then washed with 50 mM sodium bicarbonate (pH 9.0) for three times. The paper was air dried and the amount of radioactivity incorporated into the peptide substrate was quantified by liquid scintillation counting. |
| Cell experiment [1]: | |
|
Cell lines |
HeLa cells |
|
Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Applications |
MG 149 inhibited the activity of HAT in nuclear extracts from HeLa cells using biotinylated histone H3 or histone H4 peptides as substrates. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Ghizzoni M, Wu J, Gao T, Haisma HJ, Dekker FJ, George Zheng Y. 6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site. Eur J Med Chem. 2012 Jan;47(1):337-44. |
|
MG 149 is an inhibitor of histone acetyltransferases (HAT) with IC50 values of 74μM and 47μM for Tip60 and MOF, respectively [1].
MG 149 is an anacardic acid derivative. It shows selective inhibition towards the MYST type of HATs: Tip60 and MOF with IC50 values of 74μM and 47μM, respectively. The docking study shows that the inhibition of Tip60 by MG 149 is competitive with respect to Ac-CoA in the Ac-CoA binding pocket of Tip60. MG 149 also inhibits the activity of HAT in nuclear extracts from HeLa cells using biotinylated histone H3 or histone H4 peptides as substrates. It is found to be more potent for histone H3 compared to histone H4. Additionally, DNA microarrays demonstrate that MG149 inhibits p53 and NF-kB pathways as well as a very limited number of other pathways [1, 2].
References:
[1] Ghizzoni M, Wu J, Gao T, Haisma HJ, Dekker FJ, George Zheng Y. 6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site. Eur J Med Chem. 2012 Jan;47(1):337-44.
[2] Dekker FJ, van den Bosch T, Martin NI. Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases. Drug Discov Today. 2014 May;19(5):654-60.
| Cas No. | 1243583-85-8 | SDF | |
| 别名 | Tip60 HAT inhibitor | ||
| 化学名 | 2-(4-heptylphenethyl)-6-hydroxybenzoic acid | ||
| Canonical SMILES | CCCCCCCC1=CC=C(CCC2=C(C(O)=O)C(O)=CC=C2)C=C1 | ||
| 分子式 | C22H28O3 | 分子量 | 340.46 |
| 溶解度 | ≥ 114mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9372 mL | 14.686 mL | 29.372 mL |
| 5 mM | 0.5874 mL | 2.9372 mL | 5.8744 mL |
| 10 mM | 0.2937 mL | 1.4686 mL | 2.9372 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。